
CAS Name: 4-Isothiocyanato-N-(4-nitrophenyl)benzeneamine
Additional Names: isothiocyanic acid p-(p-nitroanilino)phenyl ester; 4-isothiocyanato-4'-nitrodiphenylamine; nithiocyaminePercent Compos...
Literature References: Analog of nitroscanate, q.v. Prepn: K. Antos et al., DE 1932690 (1970 to Cesk. Akad. Ved), C.A. 72, 100265 (1970); S. Rajappa et al., J. Chem. Soc. Perkin Trans. 1 1979, 2001; N. Viswanathan, R. C. Desai, Indian J. Chem. 20B, 308 (1981). Anthelmintic activity: H. P. Striebel, Experientia 32, 457 (1976); K. R. Middleton et al., ibid. 35, 243 (1979); H. G. Sen, B. N. Deb, Am. J. Trop. Med. Hyg. 30, 992 (1981). HPLC determn in human plasma: W. M. Kofi-Tsekpo, C. W. Karekezi, Drugs Exp. Clin. Res. 14, 31 (1988). Clinical pharmacology: A. B. Vaidya et al., Br. J. Clin. Pharmacol. 4, 463 (1977). Mutagenicity study: B. S. Reddy et al., Antimicrob. Agents Chemother. 22, 707 (1982). Brief review: J. I. Bruce, Int. J. Parasitol. 17, 131-140 (1987).
CAS Name: 1-Butanoic acid-7-glycine-1,6-dicarbaoxytocin
Additional Names: 1-butyric acid-6-(L-2-aminobutyric acid)-7-glycineoxytocin; 7-glycine-1,6-aminosuberic acid-oxytocin; [Gly7,Asu1,6]oxyt...
Literature References: Analog of oxytocin, q.v. Prepn: S. Sakakibara et al., DE 2056298; eidem, US 3749705 (1971, 1973 both to Yoshitomi). Synthesis and uterotonic activity: T. Yamanaka, S. Sakakibara, Bull. Chem. Soc. Jpn. 47, 1228 (1974). Pharmacological and biochemical properties: T. Oka et al., Jpn. J. Pharmacol. 25, 15 (1975). Comparison with prostaglandin F2a as oxytocic: T. Hashimoto, Iryo 30, 1121 (1976), C.A. 87, 554e (1977). Distribution, metabolism, excretion: Y. Kato et al., Iyakuhin Kenkyu 12, 433 (1981), C.A. 95, 126386k (1981). Teratogenicity studies: Y. Hamada et al., ibid. 10, 26, 41 (1979), C.A. 91, 639u, 83856m (1979).
CAS Name: 4-Hydroxy-2-oxo-1-pyrrolidineacetamide
Additional Names: 2-(4-hydroxypyrrolidin-2-on-1-yl)acetamide; hydroxypiracetamTrademarks: Neuractiv (Novartis); Neuromet (SKB)
Percent Compos...
Literature References: Analog of piracetam, q.v., with psychostimulant activity. Prepn: G. Pifferi, M. Pinza, DE 2635853; eidem, US 4118396 (1977, 1978 both to I.S.F.); eidem, Farmaco Ed. Sci. 32, 602 (1977). Effect on learning and memory in animals and prepn of enantiomers: S. Banfi et al., ibid. 39, 16 (1984). Effect in animals with cerebral impairment: S. Banfi et al., Pharmacol. Res. Commun. 16, 67 (1984). Pharmacokinetics in humans: E. Perucca et al., Eur. J. Drug Metab. Pharmacokinet. 9, 267 (1984). Clinical evaluation in organic brain syndrome: B. Saletu et al., Neuropsychobiology 13, 44 (1985).
CAS Name: N4-[2,6-Dimethoxy-4-methyl-5-[3-(trifluoromethyl)phenoxy]-8-quinolinyl]-1,4-pentanediamine
Additional Names: 8-[(4-amino-1-methylbutyl)amino]-2,6-dimethoxy-4-methyl-5-[3-(trifluoromet...
Literature References: Analog of primaquine, q.v. Prepn: P. Blumbergs, M. P. LaMontagne, US 4617394 (1986 to U.S. Sec. Army); M. P. LaMontagne et al., J. Med. Chem. 32, 1728 (1989). HPLC determn in blood and plasma: D. A. Kocisko et al., Ther. Drug Monit. 22, 184 (2000). Metabolism: O. R. Idowu et al., Drug Metab. Dispos. 23, 1 (1995). Clinical pharmacokinetics: M. D. Edstein et al., Br. J. Pharmacol. 52, 663 (2001). Clinical evaluation in prevention of malaria relapse: D. S. Walsh et al., J. Infect. Dis. 180, 1282 (1999); in malaria prophylaxis: B. Lell et al., Lancet 355, 2041 (2000); B. R. Hale et al., Clin. Infect. Dis. 36, 541 (2003).
CAS Name: (5Z)-7-[(1R,2R,3R)-3-Hydroxy-2-[(1E,3R)-3-hydroxy-4-phenoxy-1-butenyl]-5-oxocyclopentyl]-N-(methylsulfonyl)-5-heptenamideTrademarks: Nalador (Schering AG)
Percent Composition: C 59.34...
Literature References: Analog of prostaglandin E2, q.v., with uterine stimulant activity. Prepn: J. Bindra, M. R. Johnson, DE 2355540 (1974 to Pfizer), C.A. 81, 49330u (1974); eidem, US 4024179 (1977 to Pfizer). Antifertility effects: H. Hess et al., Experientia 33, 1076 (1977). Influence on platelet function: R. C. Briel, T. H. Lippert, Adv. Prostaglandin Thromboxane Res. 6, 351 (1980). Biological action and half-life: eidem, Prostaglandins Med. 6, 1 (1981). Induction of abortion: K. Schmidt-Gollwitzer, Int. J. Fertil. 26, 86 (1981).
CAS Name: (5Z,9a,11a,13E,15S)-9,11,15-Trihydroxy-15-methylprosta-5,13-dien-1-oic acid
Additional Names: 7-[3,5-dihydroxy-2-(3-hydroxy-3-methyl-1-octenyl)cyclopentyl]-5-heptenoic acid; (15S)-15-...
Literature References: Analog of prostaglandin F2a, q.v. Prepn: G. L. Bundy et al., DE 2121980; G. L. Bundy, US 3728382 (1971, 1973 both to Upjohn); eidem, Ann. N.Y. Acad. Sci. 180, 76 (1971); E. W. Yankee et al., J. Am. Chem. Soc. 96, 5865 (1974). Biological activity: J. R. Weeks et al., J. Pharmacol. Exp. Ther. 186, 67 (1973). Mechanism of action: A. I. Csapo, M. O. Pulkkinen, Prostaglandins 18, 479 (1979). Clinical studies: P. C. Schwallie, K. R. Lamborn, J. Reprod. Med. 23, 289 (1979); M. P. Mapa et al., Int. J. Gynaecol. Obstet. 20, 125 (1982). Teratological study: G. M. Szczech et al., Adv. Prostaglandin Thromboxane Res. 4, 157 (1978).
CAS Name: (E)-3-[2-(1,4,5,6-Tetrahydro-1-methyl-2-pyrimidinyl)ethenyl]phenol
Additional Names: (E)-m-[2-(1,4,5,6-tetrahydro-1-methyl-2-pyrimidinyl)vinyl]phenol; 1-methyl-1,4,5,6-tetrahydro-2-[2...
Literature References: Analog of pyrantel, q.v., with activity vs whipworms (Trichuris spp.). Prepn: J. W. Mc Farland, ZA 6804589 corresp to US 3579510 and US 3708584 (1968, 1971, 1973 all to Pfizer). Synthesis and evaluation in whipworm control: J. W. Mc Farland, H. L. Howes J. Med. Chem. 15, 365 (1972). Evaluation vs Trichuris in dogs: H. L. Howes, Proc. Soc. Exp. Biol. Med. 139, 394 (1972). Efficacy vs T. trichiuris in humans: E. L. Lee et al., Am. J. Trop. Med. Hyg. 25, 563 (1976); vs T. suis in swine: M. Robinson, Vet. Parasitol. 5, 223 (1979). Anthelmintic effects of combination with pyrantel pamoate: B. Sinniah, D. Sinniah, Ann. Trop. Med. Parasitol. 75, 315 (1981).
CAS Name: [3b,16b,17a,18b,20a]-18-[[(2E)-3-(4-Hydroxy-3-methoxyphenyl)-1-oxo-2-propenyl]oxy]-11,17-dimethoxyyohimban-16-carboxylic acid methyl ester
Additional Names: methyl O-(4-hydroxy-3-meth...
Literature References: Analog of rescinnamine. Prepn: BE 782661 corresp to T. Kametani, US 3898215 (1972, 1975 both to Nippon Chemiphar); T. Kametani et al., J. Med. Chem. 15, 686 (1972). Mass spectrum: eidem, J. Chem. Soc. Perkin Trans. 1 1975, 932. Antihypertensive activity: H. Kato et al., Jpn. J. Pharmacol. 27, 87 (1977). Effects on respiration, cardiovascular system, renal function: T. Kamishiro et al., Oyo Yakuri 20, 441 (1980), C.A. 96, 28430w (1982). Toxicity study: T. Fukuda et al., ibid. 18, 71 (1979), C.A. 92, 104392v (1980).
CAS Name: (8S,10S)-10-[(3-Amino-2,3,6-trideoxy-a-L-arabino-hexopyranosyl)oxy]-7,8,9,10-tetrahydro-6,8,11-trihydroxy-8-(hydroxyacetyl)-1-methoxy-5,12-naphthacenedione
Additional Names: 3-glycolo...
Literature References: Analog of the anthracycline antibiotic doxorubicin, q.v., differing only in the position of the C-4 hydroxy group of the sugar moiety. Prepn: F. Arcamone et al., DE 2510866; eidem, US 4058519 (1975, 1977 both to Soc. Farmaceut. Italia); eidem, J. Med. Chem. 18, 703 (1975); S. Penco, Process Biochem. 15(5), 12 (1980). Purification: E. Oppici et al., BE 898506; eidem, GB 2133005 (both 1984 to Farmitalia Carlo Erba). Comparison with doxorubicin of in vitro activity: A. Di Marco et al., Cancer Res. 36, 1962 (1976). Tissue distribution: C. Italia et al., Br. J. Cancer 47, 545 (1983); F. Arcamone et al., Cancer Chemother. Pharmacol. 12, 157 (1984). HPLC determn in biological fluids: P. E. Deesen, B. Leyland-Jones, Drug Metab. Dispos. 12, 9 (1984); G. Cassinelli et al., ibid. 506. Clinical trials in solid tumors: K. Kolaric et al., J. Cancer Res. Clin. Oncol. 106, 148 (1983). Review of activity in experimental tumors: A. Goldin et al., Invest. New Drugs 3, 3-21 (1985). Review of pharmacology and clinical efficacy: F. Ganzina, Cancer Treat. Rev. 10, 1-22 (1983); R. J. Cersosimo, W. K. Hong, J. Clin. Oncol. 4, 425-439 (1986); P. Hurteloup, F. Ganzina, Drugs Exp. Clin. Res. 13, 233-246 (1986). Review of epirubicin and other anthracycline antineoplastics: R. B. Weiss et al., Cancer Chemother. Pharmacol. 18, 185-97 (1986).
CAS Name: 2',3'-Didehydro-3'-deoxythymidine
Additional Names: 1-(2,3-dideoxy-b-glycero-pent-2-enofuranosyl)thymine; 3'-deoxy-2'-thymidinene; D4TTrademarks: Zerit (BMS)
Percent Composition: C...
Literature References: Analog of thymidine, q.v.; reverse transcriptase inhibitor. Prepn: J. P. Horwitz et al., J. Org. Chem. 31, 205 (1966); J. W. Beach et al., ibid. 57, 3887 (1992). Large scale production: J. E. Starrett et al., EP 334368; eidem, US 5130421 (1989, 1992 both to Bristol-Myers). In vitro activity against HIV and toxicology: M. M. Mansuri et al., Antimicrob. Agents Chemother. 34, 637 (1990). Mechanism of action study: H.-T. Ho, M. J. M. Hitchcock, ibid. 33, 844 (1989). Disposition and metabolism: E. M. Cretton et al., ibid. 37, 1816 (1993). Clinical pharmacokinetics: M. N. Dudley et al., J. Infect. Dis. 166, 480 (1992). HPLC determn in plasma and urine: J. S. Janiszewski et al., J. Chromatogr. 577, 151 (1992). Clinical evaluation in AIDS and ARC: M. J. Browne et al., J. Infect. Dis. 167, 21 (1993).
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